Protein kinase C (PKC) is a family of phosplolipid-dependent serine/threonine-specific protein kinases which play an important role in cellular growth control, regulation and differentiation.
Since the activation of PKC has been implicated in several human disease processes, including various forms of cancer, different forms of inflammatory and/or immunological disorders as well as some neurological disorders, inhibition of PKC could be therapeutic value in treating these conditions.
Several classes of compounds have been identified as PKC inhibitors, e.g., isoquinoline sulfonamides, sphingosine and related sphingolipids and indolocarbazoles.
EP, B1, 0328026 discloses the use of certain bisindolylmaleimides, a class of compounds related to the indolocarbazoles, in medicaments for the treatment of various diseases.
Little work has been done on the design of PKC inhibitors with a favorable topical/systemic effect ratio. In fact, PKC is an ubiquitous enzyme with wide-ranging physiological functions, and the use of non-specific PKC inhibitors would be expected to be accompanied by severe systemic side effects.